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TEBIPENEM PIVOXIL

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TEBIPENEM PIVOXIL Basic information

Product Name:
TEBIPENEM PIVOXIL
Synonyms:
  • (1R,5S,6S)-6-[1(R)-Hydroxyethyl]-1-methyl-2-[1-(2-thiazolin-2-yl)azetidin-3-ylsulfanyl]-1-carba-2-penem-3-carboxylic acid pivaloyloxymethyl ester
  • Tebipenem Pivoxil
  • [(2,2-Dimethylpropanoyl)oxy]methyl (4R,5S,6S)-3-{[1-(4,5-dihydro-1,3-thiazol-2-yl)azetidin-3-yl]sulfanyl}-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate
  • (4R,5S,6S)-3-[[1-(4,5-Dihydro-2-thiazolyl)-3-azetidinyl]thio]-6-[(1R)-1-hydroxyethyl]-4-Methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic Acid (2,2-DiMethyl-1-oxopropoxy)Methyl Ester
  • [4R-[4α,5β,6β(R*)]]-3-[[1-(4,5-Dihydro-2-thiazolyl)-3-azetidinyl]thio]-6-(1-hydroxyethyl)-4-Methyl-7-oxo-1-Azabicyclo[3.2.0]hept-2-ene-2-carboxylic Acid (2,2-DiMethyl-1-oxopropoxy)Methyl Ester
  • OrapeneM
  • ME1211
  • TBPM-PI
CAS:
161715-24-8
MF:
C22H31N3O6S2
MW:
497.63
EINECS:
1308068-626-2
Product Categories:
  • Inhibitors
  • API
Mol File:
161715-24-8.mol
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TEBIPENEM PIVOXIL Chemical Properties

Melting point:
140-142℃
Boiling point:
661.9±65.0 °C(Predicted)
Density 
1.50
storage temp. 
Sealed in dry,Store in freezer, under -20°C
solubility 
Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly)
pka
14.36±0.20(Predicted)
form 
Solid
color 
White
InChIKey
SNUDIPVBUUXCDG-QHSBEEBCSA-N
SMILES
N12[C@@]([H])([C@@H]([C@H](O)C)C1=O)[C@@H](C)C(SC1CN(C3=NCCS3)C1)=C2C(OCOC(=O)C(C)(C)C)=O
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TEBIPENEM PIVOXIL Usage And Synthesis

Chemical Properties

White Solid

Uses

Tebipenem Pivoxil is an oral carbapenem antibiotic. Tebipenem Pivoxil is absorbed and metabolized into Tebipenem, its active metabolite which showed excellent bactericidal activity against β-lactamase-nonproducing, ampicillin-resistant isolates.

Uses

Tebipenem pivoxil(L-084) is a novel oral carbapenem antibiotic with an IC50 of 100 μg/ml for human CYP isoforms. In mouse, rat, dog and monkey, TBPM-PI were absorbed quickly, and the bioavailability was (71.4, 59.1, 34.8 and 44.9%, respectively. There was

Definition

ChEBI: Tebipenem pivoxil is a member of carbapenems and a pivaloyloxymethyl ester.

Biological Activity

Tebipenem pivoxil (L-084I; ME1211; SPR994; Tebi-pivoxil; TBM-PI) corresponds to the orally bioavailable pivalyl ester prodrug form of the carbapenem class broad-spectrum β-lactam antibiotic Tebipenem (LJC 11,036; SPR859; TBM). TBM is potent against both gram-positive and gram-negative bacteria, including penicillin-resistant S. pneumoniae (PRSP) and many β-lactamase-producing strains, while being less effective against methicillin-resistant S. aureus (MRSA), S. marcescens, and P. aeruginosa. TBM is 2- to 64-fold more potent than imipenem, cefdinir, and faropenem against clinical isolates from respiratory and urinary-tract infections.

in vivo

Tebipenem pivoxil (L084) (0-4.00 g/kg; p.o.; once) shows minimal lethal dosage (MLD) of 4.00 g/kg and the maximum tolerance dosage (MTD) of 3.40 g/kg in mice[1].
Tebipenem pivoxil (50 and 100 mg/kg; p.o.; once) significantly protects the sepsis mice challenged with various pathogenic bacteria[1].

Animal Model:KM mice weighing 18–22 g[1]
Dosage:2.89, 3.40 and 4.00 g/kg
Administration:Oral administration (tablet), once
Result:Within the 14-day observation period, only one mouse was dead in the maximum oral dosage (4.00 g/kg). The minimal lethal dosage (MLD) was 4.00 g/kg and the maximum tolerance dosage (MTD) in the mice was 3.40 g/kg. Showed dose-dependent liver and kidney damage.
Animal Model:ICR mice, sepsis mouse models[1]
Dosage:50 and 100 mg/kg
Administration:Oral administration (tablet), once
Result:Significantly increased the survival number of the sepsis mice within a 168 h observation period.

IC 50

β-lactam

TEBIPENEM PIVOXILSupplier

Taizhou KEDE Chemical Co., Ltd Gold
Tel
0576-84613060 13093829633
Email
sales@kedechemical.com
Wuhan Biocar Pharmacy Co.，Ltd Gold
Tel
18665676617
Email
2956176220@qq.com
Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
J & K SCIENTIFIC LTD.
Tel
18210857532; 18210857532
Email
jkinfo@jkchemical.com
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Email
sales@BioChemBest.com
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